反应详情

Hydrochloric acid (4 M solution in dioxane, 31.7 mL, 127 mmol) was added dropwise to a solution of tert-butyl 4-(5-amino-1H-pyrazol-3-yl)piperidine-1-carboxylate (compound described in the pamphlet of WO2011/045344, 13.5 g, 50.7 mmol) in ethyl acetate (60 mL) under ice cooling, and the mixture was stirred at room temperature for 3 hours. Ethyl acetate (40 mL) was added to the reaction solution, and the mixture was stirred for 10 minutes. Then, the obtained precipitate was collected by filtration to obtain the title compound (12.5 g, yield: 100%).

1. stirringthe mixture was stirred for 10 minutes
2. filtrationThen, the obtained precipitate was collected by filtration